Azetidines Kill Multidrug-Resistant Mycobacterium tuberculosis without Detectable Resistance by Blocking Mycolate Assembly

Azetidines Kill Multidrug-Resistant Mycobacterium tuberculosis without Detectable Resistance by Blocking Mycolate Assembly

Tuberculosis (TB) is the leading cause of global morbidity and mortality resulting from infectious disease, with over 10.6 million new cases and 1.4 million deaths in 2021. This global emergency is exacerbated by the emergence of multidrug-resistant MDR-TB and extensively drug-resistant XDR-TB; ther...

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Veröffentlicht in:Journal of medicinal chemistry 2024-02, Vol.67 (4), p.2529-2548
Hauptverfasser: Cui, Yixin, Lanne, Alice, Peng, Xudan, Browne, Edward, Bhatt, Apoorva, Coltman, Nicholas J., Craven, Philip, Cox, Liam R., Cundy, Nicholas J., Dale, Katie, Feula, Antonio, Frampton, Jon, Fung, Martin, Morton, Michael, Goff, Aaron, Salih, Mariwan, Lang, Xingfen, Li, Xingjian, Moon, Chris, Pascoe, Jordan, Portman, Vanessa, Press, Cara, Schulz-Utermoehl, Timothy, Lee, Suki, Tortorella, Micky D., Tu, Zhengchao, Underwood, Zoe E., Wang, Changwei, Yoshizawa, Akina, Zhang, Tianyu, Waddell, Simon J., Bacon, Joanna, Alderwick, Luke, Fossey, John S., Neagoie, Cleopatra
Format: Artikel
Sprache:eng
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Zusammenfassung:Tuberculosis (TB) is the leading cause of global morbidity and mortality resulting from infectious disease, with over 10.6 million new cases and 1.4 million deaths in 2021. This global emergency is exacerbated by the emergence of multidrug-resistant MDR-TB and extensively drug-resistant XDR-TB; therefore, new drugs and new drug targets are urgently required. From a whole cell phenotypic screen, a series of azetidines derivatives termed BGAz, which elicit potent bactericidal activity with MIC99 values
ISSN:0022-2623
1520-4804
1520-4804
DOI:10.1021/acs.jmedchem.3c01643